Topical pharmaceutical preparation for fever blisters and other viral infections and method of use

ABSTRACT

The present invention relates to a method and pharmaceutical composition for treating fever blisters or cold sores in mammals, and particularly in humans, by topically administering a pharmaceutical composition comprising ethyl alcohol in a concentration of at least 85% W/V and lidocaine in a concentration of 0.5-10% W/V at a periodicity of at least 10 to 12 times daily.

RELATED APPLICATIONS

This is a continuation of Ser. No. 07/846,734, filed Mar. 5, 1992, andissued as U.S. Pat. No. 5,331,012 on Jul. 19, 1994, which is acontinuation of application Ser. No. 07/559,617, filed Jul. 30, 1990 andnow abandoned.

TECHNICAL FIELD

This invention relates to a method and pharmaceutical composition fortopically treating fever blisters or cold sores and other viralinfections in mammals, and in particular in humans.

BACKGROUND ART

"Fever blisters" or "cold sores" have long been a very unpleasantmanifestation of viral Herpes-type infections. Typically, the lesionsform on the lips and/or genital area of a human and are veryuncomfortable as well as unsightly during the several week healingperiod. Since these lesions are normally of a recurring nature, a remedywhich will serve to relieve the discomfort and expedite the healingprocess has long been sought after.

In an effort to address the discomfort of fever blisters, cold sores andother lesions caused by Herpes-type viruses, many home remedies havebeen used over the years without any significant success. Also,commercial products have been developed in recent years to attempt totreat the viral infections. Representative of such products are thefollowing: CAMPHO-PHENIQUE manufactured by Winthrop Consumer Products ofNew York, N.Y.; HERPECIN-L manufactured by Campbell Labs of New York,N.Y.; and BLISTEX manufactured by Blistex Incorporated of Oakbrook, Ill.Unfortunately, none of the commercial formulations have been found to beentirely satisfactory when used as topical preparations for treatinghumans for fever blisters or cold sores and other viral infections ofboth the single occurrence as well as recurrent type.

Of interest, U.S. Pat. No. 4,628,063 to Haines et al. discloses that theuse of lidocaine, and particularly lidocaine in combination with apantothenic acid, is an effective anti-viral agent in use to treatHerpes virus infections in mammals and is particularly effective in thetreatment of HSV oral and genital lesions on humans. Haynes et al.discloses that lidocaine, a local anesthetic agent, and pantothenic acid(Vitamin B5) have an anti-viral effect on mammals, including humanbeings. It is further disclosed that lidocaine administered in the formof a pharmaceutical formulation comprising lidocaine and pantothenicacid together with a pharmaceutically acceptable carrier is particularlyeffective when injected in a single daily dosage or topically applied inan ointment or solution form 3 to 4 times daily. Unfortunately, thisformulation is not entirely satisfactory due to the inconvenience ofinjections and the lengthy time of therapy required for topicaltreatment.

DISCLOSURE OF THE INVENTION

In accordance with the present invention, applicants provide apharmaceutical composition for topically treating fever blisters or coldsores, Herpes virus infections, and other viral infections in mammals,and particularly in humans. The pharmaceutical composition comprisesethyl alcohol in a concentration of at least 85% W/V and lidocaine or apharmaceutically acceptable salt thereof in a concentration of 0.5 to10% W/V, preferably about 1-2% W/V. Optionally, the formulation may alsoinclude camphor in a concentration of 0.5 to 5% W/V, and preferablyabout 1.5% W/V. In use, the pharmaceutical composition is topicallyapplied to the infected area in an effective anti-viral amount at least10 to 12 times daily until the lesions heal.

It is therefore the object of this invention to provide an improvedpharmaceutical composition for topically treating fever blisters or coldblisters on mammals.

It is another object of the present invention to provide apharmaceutical composition for topically treating fever blisters or coldblisters, Herpes virus infections, and other viral infections whichmanifest themselves in a sore or lesion on the human body.

It is yet another object of the present invention to provide apharmaceutical composition for topically treating fever blisters or coldsores, Herpes virus infections, and other viral infections whichexpeditiously relieves the discomfort of the lesion and results in thehealing or remission of the lesion within only several days.

It is still another object of the present invention to provide apharmaceutical composition in a gel or liquid form for topical treatmentof fever or cold blisters which results in the curing or remissionthereof within 3 or 4 days when applied directly to the lesion at least10 to 12 times daily.

Some of the objects of the invention having been stated, other objectswill become evident as the description of the invention proceeds.

BEST MODE FOR CARRYING OUT THE INVENTION

Applicants have discovered that ethyl alcohol (typically 95% V/V,although other concentrations may be used, and all concentrationshereinafter being referred to as "ethyl alcohol") is an effectiveanti-viral agent for use in treating fever blisters or cold sores andother Herpes-type virus infections on mammals, and in particular onhumans, when applied directly to the lesions at least 10 to 12 timesdaily. Furthermore, applicants have discovered that the addition oflidocaine or a pharmaceutically acceptable salt thereof to the ethylalcohol significantly enhances the effectiveness of the drug.Optionally, camphor may also be added to the formulation.

Applicants are believed to be the first to discover that ethyl alcoholcan very successfully treat fever blisters or cold sores on humans whenapplied directly to the lesions at least 10 to 12 times daily, andpreferably 2 to 3 times per hour during the first day of application ofthe formulation. Although applicants believe the ethyl alcohol to beeffective without the addition of other agents to treat fever blistersor cold sores, the preferred formulation also includes lidocaine.Lidocaine (2-diethylaminoacetyl-2 6-xylidide) is known for itsproperties as a topical local anesthetic and serves to reduce the painassociated with the fever blister or cold sore lesions while the ethylalcohol acts to cause the lesions to heal or go into remission. Also,camphor may be added to the formulation and is an enhancement theretodue to its known properties as a counter-irritant.

While a pharmaceutical formulation in accordance with the presentinvention can vary, applicants presently contemplate that theformulation will comprise at least 85% W/V (by weight per unit volume)of ethyl alcohol, and lidocaine or a pharmaceutically acceptable saltthereof in a concentration of 0.5 to 10% W/V, and preferably about 1-2%W/V. Optionally, a concentration of 0.5 to 5% W/V, preferably about 1.5%W/V, of camphor may be added to the pharmaceutical formulation toenhance its counter-irritant characteristics.

LABORATORY EXAMPLES

Although many formulations are possible of the pharmaceuticalcomposition contemplated by the applicants, three preferred formulationsare set forth below. As noted above, 95% V/V ethyl alcohol was used inmaking these formulations. All formulations are for 100 ml of topicaltreatment composition, and the weight per unit volume (W/V) of eachcomponent thereof is as follows:

    ______________________________________    Formulation 1    Ethyl Alcohol                 97.5% W/V of 95% V/V Ethyl Alcohol    Lidocaine    1.0% W/V    Camphor      1.5% W/V    Total        100 ml    Formulation 2    Ethyl Alcohol                 99.0% W/V of 95% V/V Ethyl Alcohol    Lidocaine    1.0% W/V    Total        100 ml    Formulation 3    Ethyl Alcohol                 87.5% W/V of 95% V/V Ethyl Alcohol    Lidocaine    1.0% W/V    Camphor      1.5% W/V    Methylcellulose                 10.0% W/V    Total        100 ml    ______________________________________

As will be noted above, Formulation 3 contains a thickening agent,methylcellulose, in order to render the pharmaceutical composition moregel-like than the liquid solutions of Formulations 1 and 2. As a matterof choice, the pharmaceutical formulation may be a liquid solution or,if desired, 5-15% W/V of a suitable thickening agent (such asmethylcellulose) may be added to render the composition more gel-like.Whether the pharmaceutical composition of the invention is in liquid orgel form is a matter of choice, and the use of a thickening agent isconventional and known to those skilled in the art.

In use, the topical pharmaceutical formulation of the invention shouldbe applied directly to the fever blister or cold sore lesion at least 10to 12 times daily, and applications as often as every 20 minutes haveyielded very good results with no reported adverse side effects.Normally topical application of the formulation should begin at thefirst signs of a lesion and continue at the rate of 1 to 3 applicationsper hour during waking hours until the lesion is completely eradicated.Although therapy should begin as early as possible, applicants havefound that topical treatment of fully erupted fever blisters results inenhanced healing and thus believe that the formulation is effective whenapplied at any stage of lesion development.

After extensive testing on human subjects with varying types of virallesions, applicants have found the pharmaceutical formulation of t heinvention to provide unexpected and surprisingly effective results inreducing pain and facilitating healing of lesions. Although intendedprimarily for fever blisters or cold sores, applicants have found thepharmaceutical formulation to be effective with Herpes virus infectionsand believe that the formulation would also be effective in healinglesions from other related viral-type infections.

Applicants have treated a number of human subjects with thepharmaceutical formulation and had surprisingly successful results inover 90% of the cases. In the study, the patients were initially seen atvarying times after the appearance of fever blisters or cold sores andwere advised to apply the pharmaceutical treatment of the inventiondirectly to the lesion as often as possible in the morning, in theafternoon, and at night before going to bed. The results of the humancase studies indicate that the pharmaceutical formulation, topicallyapplied to lesions, is able to successfully treat fever blisters or coldsores and other viral infections in humans. Representative case studiesare set forth below:

Human Case Studies EXAMPLE 1

A 68 year old male started treatment with Formulation 1 at the firstsigns of an oral fever blister. The formulation was applied topicallyabout 6 to 7 times per day and resulted in a complete remission of thelesion in 3 days.

EXAMPLE 2

A 38 year old male had Herpes Genitalis lesions on his penis. Thepharmaceutical formulation (Formulation 2) was applied directly to thelesions 5 times daily, and complete remission was achieved in 4 days.

EXAMPLE 3

A 34 year old female who frequently experienced oral fever blisters wasusing a prescription formulation sold under the tradename ACYCLOVIR. Thepatient applied the pharmaceutical formulation of the invention(Formulation 1) as directed and reported complete remission of thelesions.

EXAMPLE 4

A 34 year old male had multiple lesions around the mouth wherein one ortwo of the lesions were fully erupted. The pharmaceutical formulation ofthe invention (Formulation 2) was applied as directed. At the end of day1 the patient reported considerable comfort improvement, and at the endof day 3 a complete remission occurred.

EXAMPLE 5

A 55 year old female had two to three day old oral lesions. Thepharmaceutical formulation (Formulation 1) was applied as directed, andcomplete remission occurred in two to three days.

EXAMPLE 6

A 60 year old male had chronic lesions and cracking of his lips for aperiod of 1 year, and his lips were reported to crack and bleedperiodically. The pharmaceutical formulation (Formulation 2) was appliedseveral times daily and relief was felt within several days and completehealing occurred in 30 days. Due to the severity of the case, thepatient experienced burning from the ethyl alcohol in the formulation,but he continued to use the formulation with no adverse side effects andreported the formulation to be excellent.

EXAMPLE 7

An 84 year old male had Herpes Zoster ("shingles") condition for severalmonths. The pharmaceutical formulation (Formulation 2) was applied 12-15times daily, and the patient reported that the burning had stopped andthe soreness and pain had been relieved over a period of 2.5 days. Thepatient reported spending about $800.00 in the previous months in anunsuccessful effort to obtain relief for his condition.

It will be understood that various details of the invention may bechanged without departing from the scope of the invention. Furthermore,the foregoing description is for the purpose of illustration only, andnot for the purpose of limitation--the invention being defined by theclaims.

What is claimed is:
 1. A pharmaceutical composition for topicallytreating fever blisters and Herpes virus infections in mammals in needof such treatment consisting essentially of:95% V/V ethyl alcohol in aconcentration of about 97.5% to about 99.0% W/V; and lidocaine or apharmaceutically acceptable salt thereof in a concentration of about1.0% to about 2.5% W/V.
 2. A method of treating fever blisters andHerpes virus infections in mammals in need of such treatment, whichconsists essentially of topically applying to the infected area aneffective anti-viral amount of a mixture consisting essentially of:95%V/V ethyl alcohol in a concentration of about 97.5% to about 99.0% W/V;and lidocaine or a pharmaceutically acceptable salt thereof in aconcentration of about 1.0% to about 2.5% W/V.